Design, synthesis and biological evaluation of imidazo[1,2‐a]pyridine analogues or derivatives as anti‐helmintic drug

Albendazole was used as the leading compound, and its structure was optimized by structural transformation and alkyl modification. 18 compounds (4a‐4r) were designed and synthesized. The in vitro and in vivo activities of the 18 compounds were determined, and the results were analyzed

Abstract

The Albendazole was used as the lead compound, which was modified by structural transformation and with alkyl groups. A total of 18 compounds(4a‐4r) were designed and synthesized.The in vitro experiment results showed thatcompounds 4e, 4f, 4k, 4l, 4q and 4r had good inhibitory effect on egg and imago of roundworm. IC₅₀ of compound 4l to anti‐egg of roundworm was 0.65±0.01 μmol/L and to anti‐imago of roundworm was 1.04±0.01 μmol/L. At the same time, it showed thatcompound 4l had the best effect in vivo, and the rate of anti‐helmintic could reach more than 99%. The acute toxicity test results showed that the LD₅₀>2100 mg·kg⁻¹ was for these compounds by oral administration, and they were belong to low toxicity compounds. In a word, compound 4l was most likely to be a new anti‐helmintic drug through screening in vitro and in vivo.

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